实验以2-(2-硝基苯基)乙腈为原料,经取代、氧化、还原、酰化四步反应合成系列N-(2-(4,6-二甲氧基嘧啶-2-羰基)苯基)取代甲酰胺类化合物,其中目标物的合成条件温和,收率64％～95％,其结构经核磁共振谱、质谱和元素分析进行确认,测定了合成化合物的除草活性.在150 g ai/hm2的剂量条件下,合成化合物无除草活性.结果表明,羰基桥连4,6-二甲氧基嘧啶与取代苯环的结构无除草活性.%The purpose of the study was to look for the novel compounds with herbicidal activities. Ten novel N-( 2-(4, 6-dimethoxypyrimidine-2-carbonyl) phenyl) substituted formamide derivatives have been synthesized using 2-(2-nitrophenyl) acetonitrile as starting material by substitution reaction, oxidation, reduction and acylation. The acylation reaction conditions were mild and the yields reached 64%- 95%. All synthesized compounds were confirmed by 1H NMR, MS and elemental analysis. The preliminary bioassays indicated that all the compounds showed no herbicidal activities at 150 g ai/hm2. The result showed that it was not feasible to replace oxygen bridge with carbonyl bridge in the structure's rebuilding and modification of pyrimidinylsalicylic acid. Similar structure's rebuilding of pyrimidinylsalicylic acid was worth further researching.
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